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Synthesis of tritium-labeled N,N-dimethyl-2-phenylaziridinium and its reaction with acetylcholinesterase

Palumaa, P.I.; Raĭdaru, G.I.; Iarv, I.L.; Shevchenko, V.P.; Miasoedov, N.F.

Bioorganicheskaia Khimiia 11(10): 1348-1352

1985

ISSN/ISBN: 0132-3423
PMID: 4074397
Document Number: 244685
The synthesis of tritium-labeled N,N-demethyl-2-phenylaziridinium has been described. The specific radioactivity of the product obtained was 1,06 TBq/mmole. Kinetics of incorporation of this radioactive label into acetylcholinesterase of cobra venom (Naja naja oxiana) has been studied at 1,05 mM ligand concentration (25 degrees C, pH 7,50. 0,15 M phosphate buffer). Under these conditions two molecules of the radioactive label have been found to react with the enzyme. One molecule incorporates fast with half-life of 4,8 min, not affecting the enzymatic activity. Incorporation of the second label is a slow reaction with half-life of 6 hr and leads to complete inactivation of acetylcholinesterase. Molecular mass of the modified enzyme is 63 +/- 4 kDa and coincides with that of native one.

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